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  3. Tucatinib

Tucatinib  (Synonyms: Irbinitinib; ARRY-380; ONT-380)

Cat. No.: HY-16069 Purity: 99.13%
COA Handling Instructions

Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

For research use only. We do not sell to patients.

Tucatinib Chemical Structure

Tucatinib Chemical Structure

CAS No. : 937263-43-9

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
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10 mg USD 90 In-stock
50 mg USD 250 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Tucatinib:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

IC50 & Target

HER2

 

In Vitro

Tucatinib has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].
Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that Tucatinib may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tucatinib (ONT-380, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose[1].
Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%)[2].
Tucatinib (ARRY-380) demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice[3].
Dosage: 200 mg/kg/d.
Administration: PO, daily.
Result: Exhibited anti-tumor activity and benefited survival.
Clinical Trial
Molecular Weight

480.52

Formula

C26H24N8O2

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (86.72 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0811 mL 10.4054 mL 20.8108 mL
5 mM 0.4162 mL 2.0811 mL 4.1622 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  30 % SBE-β-CD

    Solubility: 10 mg/mL (20.81 mM); Suspension solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.82%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0811 mL 10.4054 mL 20.8108 mL 52.0270 mL
5 mM 0.4162 mL 2.0811 mL 4.1622 mL 10.4054 mL
10 mM 0.2081 mL 1.0405 mL 2.0811 mL 5.2027 mL
15 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4685 mL
20 mM 0.1041 mL 0.5203 mL 1.0405 mL 2.6013 mL
25 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0811 mL
30 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
40 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3007 mL
50 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
60 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
80 mM 0.0260 mL 0.1301 mL 0.2601 mL 0.6503 mL
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Tucatinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tucatinib
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